ZM734
ZM734 is an orally active and selective NLRP3 inflammasome inhibitor. ZM734 inhibits the secretion of IL-1β. ZM734 alleviates pulmonary inflammation in a mouse model of acute lung injury. ZM734 can be used for the research of inflammatory diseases such as acute lung injury.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3068219-50-8
- 分子式: C19H20FN3O3S
- 分子量:389.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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IL-1β |
ZM734 (0.1-2000 nM; 1 h) potently and selectively inhibits NLRP3 inflammasome activation in mouse bone marrow-derived macrophages (BMDMs), with an IC50 value of 400 nM for IL-1β and 721 nM for IL-18, while exerting no effect on TNF-α, IL-6, AIM2 and NLRC4 pathways[1].
The CC50 of ZM734 in BMDMs is 92.0 μM[1].
ZM734 (0.1-1 μM) inhibits the production of IL-1β in human THP-1 cells[1].
ZM734 (1 μM) inhibits the expression of pro-IL-1β without altering the levels of NLRP3 or pro-caspase-1 in BMDMs stimulated with LPS (HY-D1056) + ATP (HY-B2176), and it acts on the activation stage of the NLRP3 inflammasome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs
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Concentration:0.1-10 μM; 64.5-2000 nM
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Incubation Time:1 h (pre-incubation prior to LPS stimulation)
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Result:Inhibited LPS+ATP-induced IL-1β secretion by 59.1% at 0.1 μM.
Inhibited LPS+ATP-induced IL-1β secretion by 69.5% at 1 μM.
Exhibited dose-dependent inhibition of LPS+ATP-induced IL-1β and IL-18 secretion, with IC50 values of 400 nM and 721 nM, respectively.
Did not significantly inhibit LPS-induced TNF-α or IL-6 secretion at 1 μM and 10 μM.
Significantly reduced IL-1β secretion induced by multiple NLRP3 activators (LPS+ATP, LPS+Nigericin, LPS+MSU).
Showed no significant inhibitory effect on AIM2 or NLRC4 inflammasome-mediated IL-1β secretion.
ZM734 (30-60 mg/kg; p.o.; single dose) exhibits reduced hepatotoxicity in healthy C57BL/6 mice, causing smaller elevations in serum ALT and AST levels than MCC950 at equivalent or higher oral doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (n=6 per group)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly alleviated LPS-induced lung pathological injuries, including reductions in inflammatory cell infiltration, intravascular congestion, alveolar wall thickening, and pulmonary interstitial hemorrhage.
Significantly suppressed LPS-induced increases in IL-1β levels in mouse bronchoalveolar lavage fluid, with no significant effect on TNF-α or IL-6 levels.
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Animal Model:C57BL/6 mice (8 weeks old; equal numbers of males and females; n=6 per group)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Induced smaller increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels compared to MCC950 at the same 30 mg/kg dose.
Caused ALT and AST levels that remained lower than those induced by MCC950 at 30 mg/kg when administered at 60 mg/kg.
化学情報
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CAS 番号 3068219-50-8
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分子量 389.44
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分子式 C19H20FN3O3S
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SMILES
FC1=CC(S(N/C(NC2=C3C(CCC3)=CC4=C2CCC4)=N\O)(=O)=O)=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
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